LY2828360 [Ligand Id: 12751] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL3139186 (Ly2828360, LY-2828360, LY2828360) |
|---|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| ChEMBL | Agonist activity at human CB1 receptor | B | 6 | pKi | >1000 | nM | Ki | Eur J Med Chem (2019) 165: 347-362 [PMID:30583970] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in CHO cells assessed as effect on [35S]-GTPgammaS binding after 30 mins by scintillation counting | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in Sf9 cells by [35S]-GTPgammaS binding assay | F | 4 | pEC50 | >100000 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 5572-5575 [PMID:25466177] |
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| GtoPdb | Binding affinity | - | 7.39 | pKi | 40.3 | nM | Ki | J Med Chem (2013) 56: 5722-33 [PMID:23795771] |
| ChEMBL | Binding affinity to human CB2 receptor | B | 7.4 | pKi | 40 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 5572-5575 [PMID:25466177] |
| ChEMBL | Agonist activity at human CB2 receptor | B | 7.4 | pKi | 40 | nM | Ki | Eur J Med Chem (2019) 165: 347-362 [PMID:30583970] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor transfected in CHO cells after 30 mins by liquid scintillation spectrometry | B | 7.43 | pKi | 37 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in CHO cells by [35S]-GTPgammaS binding assay | F | 7.7 | pEC50 | 20.1 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 5572-5575 [PMID:25466177] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in Sf9 membranes assessed as effect on [35S]-GTPgammaS binding after 30 mins by scintillation counting | F | 7.7 | pEC50 | 20 | nM | EC50 | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| GtoPdb | Dtermined in a GTPγS assay | - | 7.7 | pEC50 | 20.1 | nM | EC50 | J Med Chem (2013) 56: 5722-33 [PMID:23795771] |
| CB2 receptor/Cannabinoid CB2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9] | ||||||||
| ChEMBL | Displacement of [3H]-CP55940 from rat CB2 receptor by liquid scintillation spectrometry | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| ChEMBL | Binding affinity to rat CB2 receptor | B | 7.43 | pKi | 37 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 5572-5575 [PMID:25466177] |
| GtoPdb | Binding affinity | - | 7.44 | pKi | 36.7 | nM | Ki | J Med Chem (2013) 56: 5722-33 [PMID:23795771] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
